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Phase 2a > Pharmocology > Flashcards

Pharmocology Flashcards

1
Q

What are the 3 categories of drug interactions?

A

°Physiochemical
°Pharmacodynamics
°Pharmacokinetics

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2
Q

What are the types of physiochemical drug interactions?

A

°Adsorption
°Precipitation
°Chelation
°Neutralisation

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3
Q

What is the difference between pharmacodynamics and pharmacokinetics?

A 
Dynamics = DRUG affects BODY
Kinetics = BODY affects DRUG
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4
Q

In pharmacodynamics, what are the 4 ways that multiple drugs can affect the body at the same time?

A

°Summation (1+1=2)
°Synergism (1+1>2)
°Antagonism (1+1=0)
°Potentiation (1+1=1+1.5)

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5
Q

What are the 4 ways that the body can affect drug in pharmacokinetics?

A

°Absorption
°Distribution
°Metabolism
°Excretion

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6
Q

What does bioavailability mean?

A

How much of an oral drug vs how much of an IV drug is present in the system. It is calculated by the area underneath the curve when the levels are plotted on a graph

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7
Q

How does motility affect absorption?

A

Gut motility affects the rate of drug uptake and the speed at which it occurs. Drugs such as erythromycin can be given to increase gut motility

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8
Q

How does the acidity of tissues affect absorption?

A

°Drugs are split into a proportion of ionised and unionised population
°Changing the acidity to match the pH of the drug will improve motility
°E.g. a more basic environment with help the absorption of a basic drug

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9
Q

Where do drugs attach when they enter the body?

A

They can bind to proteins in the blood, tissue that are not intended and the intended tissue

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10
Q

What is the volume of distribution for a drug?

A

It is how much of the drug ends up in the area of effect. A low volume of distribution is good

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11
Q

Why can having two similar drugs in the blood stream at the same time be a bad idea sometimes?

A

If both drugs have a high level of protein binding, it can leave some of one of the drug in the blood stream. This could lead to an overdose, for example with warfarin

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12
Q

What is enzyme induction in the context of drug metabolism?

A

The pathway of CYP450 works more quickly which enhances the potency of drugs - more metabolism = more of the final product in circulation

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13
Q

What is enzyme inhibition in the context of drug metabolism?

A

The pathway of CYP450 is slowed, making the drug less effective

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14
Q

What is warfarin affected by in terms of pharmacokinetics?

A

°Protein binding levels
°Enzyme induction
°Enzyme inhibition

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15
Q

Which drugs that affect AKI can be affected by varying levels of enzymes and protein?

A

°NSAIDS
°ACE inhibitors
°Furosemide
°Gentimicin

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16
Q

How does grapefruit juice affect medication?

A

°Interacts with warfarin
°Affects protein binding
°Interacts with CYP450

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17
Q

What is draggability?

A

The ability of a protein target to bind small molecules with high affinity

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18
Q

What are 4 drug targets?

A

°Receptors
°Enzymes
°Transporters
°Ion channels

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19
Q

What is a receptor?

A

A component of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to the ligands observed effects

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20
Q

What are 4 types of drug receptor?

A

°Ligand-gated ion channels
°G-protein coupled receptors
°Kinase-linked receptors
°Nuclear receptors

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21
Q

How do ligand gated ion channels work?

A

Induce a change in the shape of the channel by the drug binding to the receptor

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22
Q

Give an example of a ligand gated ion channel

A

Nicotinic Ach receptor

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23
Q

Give an example of a GPCR

A

Muscarinic and β2 adrenoceptor.

GPCR’s usually interact with adenylate cyclase or phospholipase C

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24
Q

Give an example of a kinase linked receptor

A

Receptors for growth factors

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25
Q

Give an example of a cytosolic/nuclear receptor

A

Steroid receptors; steroids affect transcription

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26
Q

What are agonists?

A

Agonists bind to a receptor and to activate it

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27
Q

What is an antagonist?

A

Antagonists decrease the effect of an agonist. They show no response at a receptor

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28
Q

How do nuclear receptors work?

A

Gene transcription is modified. Ligands react in the cytoplasm which leads to DNA being modified in the nucleus

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29
Q

How do kinase linked receptors work?

A

Transmembrane receptors are activated when the binding of an extracellular ligand causes enzymatic activity on the intracellular side

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30
Q

What is the shape of a log dose-response curve?

A

Sigmoidal

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31
Q

What is EC50?

A

The concentration of drug that gives half the maximal response

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32
Q

What does the EC50 tell us?

A

The potency of a drug

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33
Q

Would a drug with a lower EC50 have a lower or greater potency?

A

Greater

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34
Q

What does Emax tell us about a drug?

A

The efficacy of the drug

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35
Q

How is intrinsic activity calculated?

A

Emax of partial agonist/Emax of full agonist

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36
Q

Which is more efficacious, a full agonist or partial agonist?

A

A full agonist is more efficacious because a full agonist can give a 100% response

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37
Q

What is the definition of affinity?

A

How well a ligand binds to a receptor

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38
Q

What is the definition of efficacy?

A

How well a ligand activates the receptor

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39
Q

What is an agonist to the Histamine 2 (H2) receptor and what does it do?

A

°Agonist is histamine
°Causes contraction of the ileum
°Acid secretion from parietal cells

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40
Q

What is an antagonist to the Histamine 2 (H2) receptor and what does it do?

A

°Antagonist is mepyramine
°Stops contraction of ileum
°Has no effect on acid secretion

41
Q

What is the effect of fewer receptors on drug potency?

A

Fewer receptors will shift the dose-response curve to the RHS, this means drug potency will be reduced

42
Q

What is the effect of fewer receptors on receptor response?

A

Receptor response is still 100% due to receptor reserve. (Partial agonists don’t have receptor reserve)

43
Q

What is the affect of less signal amplification on drug response?

A

Less signal amplification gives a reduced drug response

44
Q

Describe allosteric modulation

A

An allosteric modulator binds to a different site on a receptor and influences the role of an agonist

45
Q

What is inverse agonism?

A

Where an agonist has a negative effect at a receptor

46
Q

What is the definition of tolerance?

A

A reduction in the effect of a drug overtime. This can be due to continuous use of repeatedly high concentrations

47
Q

What 3 ways can a receptor be desensitised?

A

°Uncoupled (an agonist would be unable to interact with a GPCR)
°Internalised (endocytosis, the receptor is taken into vesicles in the cell)
°Degraded

48
Q

What are the two types of enzyme inhibitor?

A 
°Irreversible = react with the enzyme and changes it chemically
°Reversible = bind non-covalently and different types of inhibition occur depending on whether they bind to the enzyme or enzyme-substrate complex
49
Q

How to statins work?

A

Blocking the rate limiting step in the production of cholesterol

50
Q

What are the three types of protein port?

A

°Uniporter
°Symporter
°Antiporter

51
Q

How does a uniporter function?

A

Uses energy from ATP to pull molecules through the protein against its concentration gradient

52
Q

How does a symporter function?

A

It transports two molecules through the protein in the same direction by using the movement of one molecule to pull in another molecule against its concentration gradient

53
Q

How does an anti porter function?

A

Two molecules move in opposite directions, with one against the concentration gradient and the other one down the gradient. The energy from one going down the gradient allows the other to move in the opposite direction

54
Q

What type of porter is the Na-K-Cl (NKCC) transporter?

A

Symporter, it is used in secretory organs and in the loop of Henle in the kidney

55
Q

Can aspirin be described as a selective drug?

A

Aspirin is non-selective, it acts on COX1 and COX2

56
Q

What is the function of COX1 and COX2?

A

They cyclise and oxygenate arachidonic acid and produce prostaglandin H2

57
Q

What does prostaglandin H2 form when it interacts with synthases?

A

Prostanoids

58
Q

What is pro-drug and what is an example of one?

A

Drugs that need to be activated enzymatically e.g. ACE inhibitors, enalapril

59
Q

How do ACE inhibitors work?

A

Angiotensinogen is converted to angiotensin 1 via renin. Angiotensin 1 is then converted to angiotensin 2 via ACE. ACE inhibitors prevents angiotensin 1 binding and so you don’t get angiotensin 2 formation

60
Q

How do β lactam antibiotics work?

A

The inhibit transpeptidase and so prevent bacterial cell wall synthesis

61
Q

How do diuretics work?

A

They inhibit ‘symporters’ in the loop of Henle. This leads to increased H2O excretion and decreased salt reabsorption and so BP decreases

62
Q

What drugs work on the loop of Henle?

A

°Furosemide, act on the ascending loop.

°Thiazides, act on the distal tubule.

63
Q

How can drugs be developed?

A

°Serendipity, by chance. e.g. penicillin

°Rational drug design. e.g. propranolol

64
Q

What percentage of drugs are metabolised during the first pass through the liver?

A

50%

65
Q

What are the 3 methods of parenteral drug administration?

A

°Sub-cutaneous
°Intramuscular
°Intravenous

66
Q

How do opioids work?

A

°Work on the fight or flight response
°Opioid receptors are G-protein coupled receptors
°Opioids inhibit the release of pain transmitters at tea spinal cord and midbrain, and modulates pain perception in the higher centres of the brain

67
Q

What are the 4 types of opioid receptor?

A

MOP, KOP, NOP and DOP

68
Q

What type of opioid receptor do all current drugs use?

A

µ receptors

69
Q

What are the side effects of an opioid overdose?

A 
°Respiratory depression
°Sedation
°Nausea/vomiting
°Constipation
°Itching
°Immune suppression
°Endocrine effects
70
Q

What should you do when a patient is suffering from opioid induced respiratory depression?

A

°Call for help
°Give oxygen
°ABC
°Naloxone

71
Q

Why can codeine/tramadol be more/less effective in people?

A

It works by using the CYP2D6 gene which is over expressed in 5% of the population, leading to an increased risk of respiratory depression. Additionally, it is under-expressed/does not work in 20-25% of caucasians, leading to no effect

72
Q

What are the two main neurotransmitter?

A

°Acetylcholine

°Noradrenaline

73
Q

Which neurotransmitter do both sympathetic and parasymapthic fibres release and act on nicotinic receptors?

A

Acetylcholine

74
Q

Which neurotransmitter do post-ganglionic parasympathetic fibres release?

A

Acetylcholine which acts on the muscarinic receptors

75
Q

Which neurotransmitter do post-ganglionic sympathetic fibres release?

A

Noradrenaline which acts on alpha and beta adrenoreceptors

76
Q

What do NANC (non-adrenergic, non-cholinergic autonomic transmitters) do?

A

They work on NO and vasoactive intestinal peptide (parasympathetic) and ATP and neuropeptide Y (sympathetic)

77
Q

What/where are the muscarinic receptors?

A 
°M1 = brain
°M2 = mainly in the heart. Activation of M2 slows the heart so we can block these to reduce HR
°M3 = glandular and smooth muscle. Cause bronchoconstriction, sweating, salivary gland secretion
°M4/5 = mainly in CNS
78
Q

Name a muscarinic agonist and list its effects

A

°Pilocarpine

  • Stimulation of salivation to treat Sjogren’s
  • Contraction of smooth muscle to treat glaucoma
  • Slows the heart as a side effect
79
Q

Name two muscarine antagonists and their origins

A

°Nightshade –> atropine

°Thorn apple –> hyoscine

80
Q

Name one short acting and one long acting drug that can treat bronchoconstriction

A

°Work by blocking the M3 receptor
°Short = ipratropium bromide
°Long = LAMAs e.g. tiotropium

81
Q

What effect does acetylcholine have outside of the autonomic nervous system?

A

°ACh signalling is involved in memory
°Anti-emetic effects
°ACh also helps to innervate skeletal muscle
°Botox blocks the release of ACh

82
Q

What are the side effects of anti-cholinergic medications?

A 
°Worsening of memory
°Constipation
°Dry mouth
°Vision (blurring and glaucoma)
°Muscle paralysis (in the case of nerve gas)
83
Q

What are the 3 catecholamines?

A

°Noradrenaline = released from sympathetic nerve fibre ends
°Adrenaline = released from the adrenal glands
°Dopamine

84
Q

What is the most effective agonist of the α1 receptor, its mechanism and consequence of its activation?

A

°NAd>Ad
°Increases intracellular calcium levels and Gq signalling
°Contracts smooth muscle

85
Q

What is the most effective agonist of the α2 receptor, its mechanism and consequence of its activation?

A

°NAd=Ad
°Inhibits the cAMP family and used Gi signalling
°Mixed effects on smooth muscle

86
Q

What is the most effective agonist of the β1 receptor, its mechanism and consequence of its activation?

A

°NAd=Ad
°Increases cAMP, Gs signalling
°Chronotropic and inotropic effects on the heart

87
Q

What is the most effective agonist of the β2 receptor, its mechanism and consequence of its activation?

A

°Ad»NAd
°Increases cAMP, Gs signalling
°Relaxes smooth muscle

88
Q

What is the most effective agonist of the β3 receptor, its mechanism and consequence of its activation?

A

°NAd>Ad
°Increases cAMP, Gs signalling
°Enhances lipolysis and relaxes detrusor muscle of the bladder

89
Q

What do alpha antagonists do and why are they used?

A

°Causes vasoconstriction, especially in the skin and splanchnic region
°Used to treat septic shock
°Topical alpha activation can be used to relieve nasal decongestion

90
Q

What do alpha blockers do?

A

°Blocking α1 decreased BP - doxazosin
°Tamsulosin blocks α1A to treat prostatic hypertrophy
°There are no useful α2 blockers

91
Q

What do beta agonists do and why are they used?

A

°β1 activation increased heart rate
°β2 activation can be life saving in asthma and delaying premature labour
°β3 agonists reduce an overactive bladder

92
Q

What are some beta blockers?

A

°Propanolol blocks β1+2 to slow HR, reduce tremors

°Atenolol is β1 selective and lowers BP

93
Q

What are beta blockers used for?

A 
°Angina
°High BP
°Arrhythmia
°MI prevention
°Anxiety
°Heart failure
94
Q

What is an adverse drug reaction?

A

An unwanted or harmful reaction following administration of a drug or combination of drugs under normal use and is suspected to be related to the drug

95
Q

What are the three kinds of effect from an ADR?

A

°Toxic effect (dose > normal)
°Collateral effect (dose = normal)
°Hypersusceptibility (dose < normal)

96
Q

What do each of the Rawlins-Thompson classifications mean?

A

°Type A (augmented) - they are predictable, dose dependant and common
°Type B (bizarre) - non-predictable and not dose dependant
°Type C (continuous) - chronic
°Type D (delayed) - malignancies after immunosuppression
°Type E (end of treatment) - withdrawal
°Type F - failure of therapy

97
Q

What are the risk factors for an ADR?

A 
°Gender (F>M)
°Age
°Polypharmacy
°Genes
°Allergies
°Hepatic/renal issue
°Adherence
98
Q

What are the causes of an ADR?

A 
°Pharmaceutical variation in the drug
°Receptor abnormality
°Abnormal biological system which is revealed by the drug
°Abnormalities in drug metabolism
°Immunological causes
°Drug interaction
99
Q

What are the symptoms of anaphylaxis?

A 
°Vasodilation
°Increased vascular permeability
°Bronchoconstriction
°Urticaria
°Angio-oedema
°See ILA for more notes

Phase 2a (2 decks)

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